Rovalpituzumab tesirine
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Rovalpituzumab tesirine (SC-002) is an antibody-drug conjugate (ADC) with anticancer effects. Rovalpituzumab tesirine contains a DLL3-targeting antibody Rovalpituzumab (HY-P99043) tethered to a cytotoxic agent pyrrolobenzodiazepine by means of a protease-cleavable linker. Rovalpituzumab tesirine can be used for the stduy of small cell lung cancer (SCLC).
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- Pureté : 97.47%
- CAS No.: 1613313-09-9
- Masse moléculaire:148013 (average)
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Stockage:Shipping with dry ice
-80°C, protect from light
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Rovalpituzumab tesirine (0.01-10000 pM, 96 h) can effectively bind to mice DLL3 in KP1 cells (SCLC model) expressing mice DLL3, exhibiting potent killing effects and exerting cytotoxicity through internalization of PBD toxin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Rovalpituzumab tesirine (0.03 mg/kg, i.p once every four days) combines with anti-PD1 in the SCLC mice model leads to the infiltration and activation of CD8+ T cells in the tumor, up-regulates PD-L1 and MHC1, overcomes immunosuppression, and activates DC and STING pathways, exerting a synergistic anti-tumor effect[2].
Rovalpituzumab tesirine (0.1 mg/kg, i.p. one dose) combines with anti-PD-1 in a SCLC mice model demonstrats that CD8+ T cells are key effector cells for efficacy[2].
Rovalpituzumab tesirine (0.03 mg/kg, i.p. one dose) induces long-term antitumor immune memory in combination with anti-PD1 in a SCLC mice model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6129SF1/J mice (female, aged 6-8 weeks) injected with KP1 cells (1 × 106 cells)[2]
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Dosage:0.03 mg/kg
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Administration:i.p. one dose
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Result:Demonstrated that monotherapy or combination therapy significantly increased the proliferation and activation of CD45+ immune cells and CD8+ T cells in tumors.
Rpregulated immune activation-related genes (such as Granzyme B, IFNγ, IL-12b) and chemokines (CCL5, CXCL10) and induced PDL1 and MHC1 expression, proved the rationale for combination with anti-PD1.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1613313-09-9
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Appearance Liquid
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Masse moléculaire 148013 (average)
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Color Colorless to light yellow
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SMILES
[Rovalpituzumab tesirine]
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Synonyms
SC-002
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Livraison
Shipping with dry ice.
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Stockage
-80°C, protect from light
Pureté et documentation
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Fiche technique (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Blackhall F, et al. Efficacy and Safety of Rovalpituzumab Tesirine Compared With Topotecan as Second-Line Therapy in DLL3-High SCLC: Results From the Phase 3 TAHOE Study. J Thorac Oncol. 2021 Sep;16(9):1547-1558. [Content Brief]
[2]. Vitorino P, et al. Rova-T enhances the anti-tumor activity of anti-PD1 in a murine model of small cell lung cancer with endogenous Dll3 expression. Transl Oncol. 2021 Jan;14(1):100883. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rovalpituzumab tesirine Related Classifications
HY-132257 Related Classifications
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